TABLE 2

Cu2+ sensitivity of α subtype-mutated chimeric GABAA receptors

Receptor (αxβ3γ2L) Max Inhibition IC50nHn
% μM
α6/α1/α6(125/126;232/231)(H141R) 23.3 ± 2.3 3.8 ± 0.5 —4.0 ± 0.3 3
α1/α6/α1(126/125;231/232)(R140H) 29.0 ± 4.5 2.9 ± 0.4 —2.8 ± 0.6 5
α6/α1/α6(125/126;232/231)(V134I/R135N) 43 2.3 —2.8 1
α6/α1/α6(125/126;232/231)(V134I/R135N/H141R) 17.8 ± 2.1 2.9 ± 0.2 —2.5 ± 0.2 5
α1/α6/α1(126/125;231/232)(I133V/N134R/R140H) 41.4 ± 4.2 5